Novel substituted oxadiazole - piperazine derivatives as potential MAO inhibitors: Design, synthesis, in vitro and in silico studies

Harun Uslu; Begüm Nurpelin Saglik; Derya Osmaniye; Kadriye Benkli

Makale detayları

Novel substituted oxadiazole - piperazine derivatives as potential MAO inhibitors: Design, synthesis, in vitro and in silico studies

Yazarlar:

Harun Uslu | Begüm Nurpelin Saglik | Derya Osmaniye | Kadriye Benkli

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmaceutical Chemistry

Dergi:

Journal of Research in Pharmacy Vol.26 Issue 1, pp.20-27

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001346100

pISSN:

2630-6344

Anahtar kelimeler:

Özet:

 Recent studies have shown that there are many piperazine and oxadiazole derivatives with MAO-A andor MAO-B inhibitory activity. For this reason in our recent study, a new compound series of oxadiazole - piperazine derivatives 4a-e were designed, synthesized, characterized and screened their hMAOs inhibitory activities. When the in silico studies were examined, it was seen that the pharmacokinetic properties and interactions with the receptor of synthesized compounds were suitable. Compound 4e, with a NO2 group on the 4-position of the phenyl ring, found showing significant MAO-A inhibitory activity. Compound 4e, was the most effective agent against MAO-A enzyme with IC50 value of 0.116  0.004 μM. The newly synthesized oxadiazole - piperazine derivatives appears to be supported studies to design MAO inhibitors to obtain more suitable drugs, against diseases such as depression and anxiety due to MAO-A.

 Recent studies have shown that there are many piperazine and oxadiazole derivatives with MAO-A andor MAO-B inhibitory activity. For this reason in our recent study, a new compound series of oxadiazole - piperazine derivatives 4a-e were designed, synthesized, characterized and screened their hMAOs inhibitory activities. When the in silico studies were examined, it was seen that the pharmacokinetic properties and interactions with the receptor of synthesized compounds were suitable. Compound 4e, with a NO2 group on the 4-position of the phenyl ring, found showing significant MAO-A inhibitory activity. Compound 4e, was the most effective agent against MAO-A enzyme with IC50 value of 0.116  0.004 μM. The newly synthesized oxadiazole - piperazine derivatives appears to be supported studies to design MAO inhibitors to obtain more suitable drugs, against diseases such as depression and anxiety due to MAO-A.

 Recent studies have shown that there are many piperazine and oxadiazole derivatives with MAO-A andor MAO-B inhibitory activity. For this reason in our recent study, a new compound series of oxadiazole - piperazine derivatives 4a-e were designed, synthesized, characterized and screened their hMAOs inhibitory activities. When the in silico studies were examined, it was seen that the pharmacokinetic properties and interactions with the receptor of synthesized compounds were suitable. Compound 4e, with a NO2 group on the 4-position of the phenyl ring, found showing significant MAO-A inhibitory activity. Compound 4e, was the most effective agent against MAO-A enzyme with IC50 value of 0.116  0.004 μM. The newly synthesized oxadiazole - piperazine derivatives appears to be supported studies to design MAO inhibitors to obtain more suitable drugs, against diseases such as depression and anxiety due to MAO-A.

 Recent studies have shown that there are many piperazine and oxadiazole derivatives with MAO-A andor MAO-B inhibitory activity. For this reason in our recent study, a new compound series of oxadiazole - piperazine derivatives 4a-e were designed, synthesized, characterized and screened their hMAOs inhibitory activities. When the in silico studies were examined, it was seen that the pharmacokinetic properties and interactions with the receptor of synthesized compounds were suitable. Compound 4e, with a NO2 group on the 4-position of the phenyl ring, found showing significant MAO-A inhibitory activity. Compound 4e, was the most effective agent against MAO-A enzyme with IC50 value of 0.116  0.004 μM. The newly synthesized oxadiazole - piperazine derivatives appears to be supported studies to design MAO inhibitors to obtain more suitable drugs, against diseases such as depression and anxiety due to MAO-A.

Makale detayları

Novel substituted oxadiazole - piperazine derivatives as potential MAO inhibitors: Design, synthesis, in vitro and in silico studies

Yazarlar:

Harun Uslu | Begüm Nurpelin Saglik | Derya Osmaniye | Kadriye Benkli

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmaceutical Chemistry

Dergi:

Journal of Research in Pharmacy Vol.26 Issue 1, pp.20-27

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001346100

pISSN:

2630-6344

hMAOs inhibition

oxadiazole

piperazine

ADME

molecular docking

Sayı

Makale detayları

Novel substituted oxadiazole - piperazine derivatives as potential MAO inhibitors: Design, synthesis, in vitro and in silico studies

Yazarlar: Harun Uslu | Begüm Nurpelin Saglik | Derya Osmaniye | Kadriye Benkli

Yayıncı: Marmara University

Ana Başlıklar: Pharmaceutical Chemistry

Dergi: Journal of Research in Pharmacy Vol.26 Issue 1, pp.20-27

Belge Tipi: Makale

Yayın Tarihi: 6/2025

Belge Dili: İngilizce

Document ID (Org No.): 2001346100

pISSN: 2630-6344

hMAOs inhibition

oxadiazole

piperazine

ADME

molecular docking

Sayı

Yazarlar:

Harun Uslu | Begüm Nurpelin Saglik | Derya Osmaniye | Kadriye Benkli

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmaceutical Chemistry

Dergi:

Journal of Research in Pharmacy Vol.26 Issue 1, pp.20-27

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001346100

pISSN:

2630-6344